| | |
IC50 (nM) of uptake inhibition
|
Selectivity factor
|
|---|
|
Platelets
|
SK-N-SH
|
IC50 ratio
|
|---|
|
[3H]Serotonin
|
[125I]MIBG
|
[125I]MIBG
|
|---|
|
SSRIs
|
Alaproclate
|
516
|
38
|
43420
|
1158
|
|
Citalopram
|
32
|
7.8
|
11940
|
1521
|
|
Fluvoxamine
|
30
|
9.3
|
2339
|
252
|
|
Fluoxetine
|
115
|
32
|
1270
|
40
|
|
Norfluoxetine
|
107
|
24
|
2760
|
115
|
|
Paroxetine
|
0.6
|
0.2
|
10
|
45
|
|
Sertraline
|
41
|
36
|
3301
|
91
|
|
TCAs
|
Clomipramine
|
18
|
7
|
176
|
24
|
|
Imipramine
|
118
|
104
|
82
|
0.8
|
|
Desipramine
|
648
|
744
|
5
|
0.007
|
|
TeCA
|
Maprotiline
|
n.d.
|
1000–10,000
|
39
|
0.04–0.004
|
- Selective inhibition of 10−8 M [125I]MIBG or [3H]serotonin uptake by monoamine transporter inhibitors in human platelets or SK-N-SH neuroblastoma cells in vitro. Selectivity was expressed as the IC50 ratio of the MIBG uptake in SK-N-SH cells over that in platelets. SSRI Selective serotonin reuptake inhibitor; TCA Tricyclic antidepressant; TeCA Tetracyclic antidepressant
